# US 11,992,498 B2 · Substituted N9-adenine derivatives, pharmaceutical compositions containing same and use thereof

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- Number: US 11,992,498 B2
- Document ID: US11992498B2
- Status: Granted
- Kind: B2
- Application number: 17/254,135
- Filed: 2018-06-27
- Published: 2021-08-26
- Granted: 2024-05-28
- Earliest claimed: 2018-06-27
- Applicants: Iván Silió Oliver
- Inventors: Iván Silió Oliver
- Web page: https://patentgrep.com/patent/US11992498B2

## CPC

- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- C07F 9/65616: {containing the ring system [IMAGE cpc-sch-C07F-1006.gif] having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs}
- A61P 17/00: Drugs for dermatological disorders
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention provides new substituted N9-adenine derivatives, pharmaceutical compositions containing these derivatives and the use of the new derivatives and the pharmaceutical compositions containing same as AMPK activators, being suitable for the production of drugs for the treatment of disorders and diseases where AMPK activation plays a relevant role.

## Claims

### Claim 1

AMPK activator substituted N9-adenine derivatives having the following general formula (I)
wherein,
R is a phenyl group;
R1 and R2 are both ethyl groups;
which is N9-(3-diethylphosphonyl)phenyl-adenine.

### Claim 2 (depends on 1)

Pharmaceutical compositions containing at least one compound according to claim 1 in combination with one or several pharmaceutically acceptable excipients.

### Claim 3 (depends on 2)

Pharmaceutical compositions according to claim 2, wherein the compound is present in an effective dose of between 1 μg and 1,000 mg of the compound per kg of body weight of the subject to be treated.

### Claim 4 (depends on 3)

Pharmaceutical compositions according to claim 3, wherein the compound is present in an effective dose of between 1 mg and 300 mg per kg of body weight.

### Claim 5 (depends on 2)

A method of treating or preventing an AMPK activation-related disorder or disease in a subject comprising administering the pharmaceutical composition of claim 2 to a subject in need thereof.

### Claim 6 (depends on 5)

The method according to claim 5, wherein the AMPK activation-related disorder or disease is selected from a metabolic disease, a dermatological pathology disease, hypercholesterolemia, obesity, type 2 diabetes or metabolic syndrome, for musculoskeletal function diseases, endocrine function diseases, cellular homeostasis disease or disorders, adaptation to environmental stress.
